Dosage Form:

Composition:

Pharmacotherapeutic group:

vasodilating agent.

ATC code: [C04AD03]

Pharmacological properties
Pharmacodynamics
Parabolan steroid antispasmodic group of purines. It improves the microcirculation and blood rheology. The mechanism of action is associated with inhibition of phosphodiesterase and increase the content of cyclic AMP in platelets and ATP in erythrocytes with simultaneous saturation of energy potential, which in turn leads to vasodilatation, decreased total peripheral vascular resistance, increase in stroke and cardiac output without significant changes in heart rate ( . HR)
Expanding the coronary arteries, increases the delivery of oxygen to the myocardium (antianginal effect), pulmonary vessels – improves blood oxygenation.
increases tone of respiratory muscles (intercostal muscles and the diaphragm). When administered intravenously, it leads to increased collateral circulation, increase volume of blood flowing through a unit cross section. It leads to an increase in ATP content in the brain, a positive effect on the bioelectric activity of the central nervous system.
Reduces blood viscosity, increases the elasticity of erythrocyte membranes (due to the impact on pathologically altered deformability of red blood cells). It improves the microcirculation in the areas of impaired circulation.
In peripheral arterial occlusive disease ( “intermittent” claudication) leads to a lengthening of the distance away, elimination of night leg cramps and pain at rest.

PharmacokineticsThe drug is rapidly metabolized in the liver. During metabolism several active metabolites are formed, which are of major metabolite metabolite 1 and 5. Their blood plasma concentrations of 5 and 8 times (respectively) above concentration of the starting material.
Displayed as metabolites (94%) and in the intestine (4% ), the first output chasa 4 to 90% of the dose. The unchanged output 2% of the drug. parabolan steroid and its metabolites do not bind to plasma proteins.
Excretion slowed metabolites In severe renal dysfunction. If abnormal liver function observed lengthening half-life and increased bioavailability parabolan side effects.

Indications

the peripheral blood circulation against the background of atherosclerosis, diabetes and inflammatory processes (including in the “intermittent” claudication due to atherosclerosis, diabetic angiopathy, obliterative endarteritis);

trophic disorders of tissues as a result of violations of arterial or venous microcirculation (varicose ulcers, gangrene, frostbite);

Hypersensitivity to parabolan steroid and substances from the group of xanthine derivatives;

pronounced coronary or cerebral arteriosclerosis;

acute myocardial infarction;

The expressed disturbances of heart rhythm;

uncontrolled arterial hypotension;

porphyria;

massive bleeding;

retinal hemorrhage;

acute hemorrhagic stroke;

pregnancy, lactation;

age of 18 years (effectiveness and safety have been established). With care – patients with labile blood pressure, prone to hypotension, congestive heart failure, a tendency to hemorrhage, state after recently transferred surgical intervention, liver and / or kidney failure. Dosing and Administration
The drug can be administered intravenously, intraarterially, intramuscularly.
During the infusion the patient should be in a prone position. Intravenously – 100 mg (1 ampoule) in 250-500 mL of 0.9% sodium chloride solution or 5% dextrose solution ( glucose) infusion over 1.5-3 hours.With good tolerance dose can be increased to 100 mg per day. The maximum daily dose of -300 mg. Intraarterially – 100 mg of the drug initially in 20-50 ml of 0.9% sodium chloride solution in the following days – 200-300 30-50 mg per ml of solvent. Administered at 100 mg (5 ml of a 2% solution of the drug) over 10 minutes. When atherosclerosis of cerebral vessels can not enter into the carotid artery. Patients with chronic renal insufficiency (creatinine clearance less than 10 mL / min) was administered to 50-70% of the usual dose. Intramuscular: 1-2 times a day with 100 mg (1 ampoule ). Side effect On the part of the central nervous system: headache, dizziness; anxiety, sleep disorders, convulsions. Cardio-vascular system: tachycardia, arrhythmia, cardialgia rarely -progressirovanie angina, lower blood pressure. For the skin: facial flushing, “tides” of blood to the skin of the face and upper chest cell swelling, increased fragility of nails. On the part of the digestive tract: nausea, vomiting, feeling of heaviness in the stomach, loss of appetite, intestinal atony, aggravation cholecystitis, cholestatic hepatitis, bleeding from the mucous membranes of the stomach membranes tren side effects, the intestines. from the senses: blurred vision, scotoma. On the part of the hemostatic system and of hematopoiesis: thrombocytopenia, leukopenia, pancytopenia, gipofibrinogenemia; bleeding from vessels in the skin. Allergic reactions: rarely – itching, skin flushing, urticaria, angioedema, anaphylactic shock. Laboratory findings: increased activity of “liver” enzymes: alanine aminotransferase (ALT), aspartate aminotransferase (the ACT), lactate dehydrogenase (LDH) and alkaline phosphatase .Overdose symptoms: weakness, dizziness, marked reduction in blood pressure, fainting, tachycardia, drowsiness, loss of consciousness, tonic-clonic seizures, increased nervous irritability, pyrexia, areflexia, signs of gastrointestinal bleeding (vomiting-type “coffee grounds”). Treatment : symptomatic aimed at maintaining respiratory function and blood pressure.Interaction with other drugs
parabolan steroid may increase the effects of drugs that affect blood clotting (indirect and direct anticoagulants, thrombolytics) anitibiotikov (including cephalosporins – tsefamandola, cefoperazone, tsefotetan)., Valproic acid
increases the effectiveness of antihypertensive drugs, insulin and oral hypoglycemic agents.
Cimetidine increases the concentration of parabolan steroid in plasma (the risk of side effects).
Co-administration with other xanthines can lead to excessive nervous excitement.

Specific guidance
Treatment should be under the control of blood pressure. In patients with chronic heart failure should be to achieve compensation of blood circulation.
In patients with diabetes, taking hypoglycemic agents, the appointment of large doses can cause pronounced hypoglycemia (dose correction is required).
When assigning simultaneously with anticoagulants should be carefully monitored for indicators of blood coagulation. In patients who have undergone recent surgery, requires systematic monitoring of hemoglobin concentration and hematocrit.
The dose should be reduced in patients with low and unstable blood pressure. Older people may require dose reduction (decreased clearance rate).
Smoking may reduce the therapeutic efficacy of the drug. Compatibility parabolan steroid solution with another infusion solution should be checked in each case.